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Pharmocology Flashcards

1
Q

What are the 3 categories of drug interactions?

A

°Physiochemical
°Pharmacodynamics
°Pharmacokinetics

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2
Q

What are the types of physiochemical drug interactions?

A

°Adsorption
°Precipitation
°Chelation
°Neutralisation

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3
Q

What is the difference between pharmacodynamics and pharmacokinetics?

A 
Dynamics = DRUG affects BODY
Kinetics = BODY affects DRUG
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4
Q

In pharmacodynamics, what are the 4 ways that multiple drugs can affect the body at the same time?

A

°Summation (1+1=2)
°Synergism (1+1>2)
°Antagonism (1+1=0)
°Potentiation (1+1=1+1.5)

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5
Q

What are the 4 ways that the body can affect drug in pharmacokinetics?

A

°Absorption
°Distribution
°Metabolism
°Excretion

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6
Q

What does bioavailability mean?

A

How much of an oral drug vs how much of an IV drug is present in the system. It is calculated by the area underneath the curve when the levels are plotted on a graph

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7
Q

How does motility affect absorption?

A

Gut motility affects the rate of drug uptake and the speed at which it occurs. Drugs such as erythromycin can be given to increase gut motility

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8
Q

How does the acidity of tissues affect absorption?

A

°Drugs are split into a proportion of ionised and unionised population
°Changing the acidity to match the pH of the drug will improve motility
°E.g. a more basic environment with help the absorption of a basic drug

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9
Q

Where do drugs attach when they enter the body?

A

They can bind to proteins in the blood, tissue that are not intended and the intended tissue

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10
Q

What is the volume of distribution for a drug?

A

It is how much of the drug ends up in the area of effect. A low volume of distribution is good

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11
Q

Why can having two similar drugs in the blood stream at the same time be a bad idea sometimes?

A

If both drugs have a high level of protein binding, it can leave some of one of the drug in the blood stream. This could lead to an overdose, for example with warfarin

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12
Q

What is enzyme induction in the context of drug metabolism?

A

The pathway of CYP450 works more quickly which enhances the potency of drugs - more metabolism = more of the final product in circulation

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13
Q

What is enzyme inhibition in the context of drug metabolism?

A

The pathway of CYP450 is slowed, making the drug less effective

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14
Q

What is warfarin affected by in terms of pharmacokinetics?

A

°Protein binding levels
°Enzyme induction
°Enzyme inhibition

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15
Q

Which drugs that affect AKI can be affected by varying levels of enzymes and protein?

A

°NSAIDS
°ACE inhibitors
°Furosemide
°Gentimicin

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16
Q

How does grapefruit juice affect medication?

A

°Interacts with warfarin
°Affects protein binding
°Interacts with CYP450

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17
Q

What is draggability?

A

The ability of a protein target to bind small molecules with high affinity

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18
Q

What are 4 drug targets?

A

°Receptors
°Enzymes
°Transporters
°Ion channels

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19
Q

What is a receptor?

A

A component of a cell that interacts with a specific ligand and initiates a change of biochemical events leading to the ligands observed effects

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20
Q

What are 4 types of drug receptor?

A

°Ligand-gated ion channels
°G-protein coupled receptors
°Kinase-linked receptors
°Nuclear receptors

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21
Q

How do ligand gated ion channels work?

A

Induce a change in the shape of the channel by the drug binding to the receptor

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22
Q

Give an example of a ligand gated ion channel

A

Nicotinic Ach receptor

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23
Q

Give an example of a GPCR

A

Muscarinic and β2 adrenoceptor.

GPCR’s usually interact with adenylate cyclase or phospholipase C

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24
Q

Give an example of a kinase linked receptor

A

Receptors for growth factors

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25
Give an example of a cytosolic/nuclear receptor
Steroid receptors; steroids affect transcription
26
What are agonists?
Agonists bind to a receptor and to activate it
27
What is an antagonist?
Antagonists decrease the effect of an agonist. They show no response at a receptor
28
How do nuclear receptors work?
Gene transcription is modified. Ligands react in the cytoplasm which leads to DNA being modified in the nucleus
29
How do kinase linked receptors work?
Transmembrane receptors are activated when the binding of an extracellular ligand causes enzymatic activity on the intracellular side
30
What is the shape of a log dose-response curve?
Sigmoidal
31
What is EC50?
The concentration of drug that gives half the maximal response
32
What does the EC50 tell us?
The potency of a drug
33
Would a drug with a lower EC50 have a lower or greater potency?
Greater
34
What does Emax tell us about a drug?
The efficacy of the drug
35
How is intrinsic activity calculated?
Emax of partial agonist/Emax of full agonist
36
Which is more efficacious, a full agonist or partial agonist?
A full agonist is more efficacious because a full agonist can give a 100% response
37
What is the definition of affinity?
How well a ligand binds to a receptor
38
What is the definition of efficacy?
How well a ligand activates the receptor
39
What is an agonist to the Histamine 2 (H2) receptor and what does it do?
°Agonist is histamine °Causes contraction of the ileum °Acid secretion from parietal cells
40
What is an antagonist to the Histamine 2 (H2) receptor and what does it do?
°Antagonist is mepyramine °Stops contraction of ileum °Has no effect on acid secretion
41
What is the effect of fewer receptors on drug potency?
Fewer receptors will shift the dose-response curve to the RHS, this means drug potency will be reduced
42
What is the effect of fewer receptors on receptor response?
Receptor response is still 100% due to receptor reserve. (Partial agonists don't have receptor reserve)
43
What is the affect of less signal amplification on drug response?
Less signal amplification gives a reduced drug response
44
Describe allosteric modulation
An allosteric modulator binds to a different site on a receptor and influences the role of an agonist
45
What is inverse agonism?
Where an agonist has a negative effect at a receptor
46
What is the definition of tolerance?
A reduction in the effect of a drug overtime. This can be due to continuous use of repeatedly high concentrations
47
What 3 ways can a receptor be desensitised?
°Uncoupled (an agonist would be unable to interact with a GPCR) °Internalised (endocytosis, the receptor is taken into vesicles in the cell) °Degraded
48
What are the two types of enzyme inhibitor?
``` °Irreversible = react with the enzyme and changes it chemically °Reversible = bind non-covalently and different types of inhibition occur depending on whether they bind to the enzyme or enzyme-substrate complex ```
49
How to statins work?
Blocking the rate limiting step in the production of cholesterol
50
What are the three types of protein port?
°Uniporter °Symporter °Antiporter
51
How does a uniporter function?
Uses energy from ATP to pull molecules through the protein against its concentration gradient
52
How does a symporter function?
It transports two molecules through the protein in the same direction by using the movement of one molecule to pull in another molecule against its concentration gradient
53
How does an anti porter function?
Two molecules move in opposite directions, with one against the concentration gradient and the other one down the gradient. The energy from one going down the gradient allows the other to move in the opposite direction
54
What type of porter is the Na-K-Cl (NKCC) transporter?
Symporter, it is used in secretory organs and in the loop of Henle in the kidney
55
Can aspirin be described as a selective drug?
Aspirin is non-selective, it acts on COX1 and COX2
56
What is the function of COX1 and COX2?
They cyclise and oxygenate arachidonic acid and produce prostaglandin H2
57
What does prostaglandin H2 form when it interacts with synthases?
Prostanoids
58
What is pro-drug and what is an example of one?
Drugs that need to be activated enzymatically e.g. ACE inhibitors, enalapril
59
How do ACE inhibitors work?
Angiotensinogen is converted to angiotensin 1 via renin. Angiotensin 1 is then converted to angiotensin 2 via ACE. ACE inhibitors prevents angiotensin 1 binding and so you don't get angiotensin 2 formation
60
How do β lactam antibiotics work?
The inhibit transpeptidase and so prevent bacterial cell wall synthesis
61
How do diuretics work?
They inhibit 'symporters' in the loop of Henle. This leads to increased H2O excretion and decreased salt reabsorption and so BP decreases
62
What drugs work on the loop of Henle?
°Furosemide, act on the ascending loop. | °Thiazides, act on the distal tubule.
63
How can drugs be developed?
°Serendipity, by chance. e.g. penicillin | °Rational drug design. e.g. propranolol
64
What percentage of drugs are metabolised during the first pass through the liver?
50%
65
What are the 3 methods of parenteral drug administration?
°Sub-cutaneous °Intramuscular °Intravenous
66
How do opioids work?
°Work on the fight or flight response °Opioid receptors are G-protein coupled receptors °Opioids inhibit the release of pain transmitters at tea spinal cord and midbrain, and modulates pain perception in the higher centres of the brain
67
What are the 4 types of opioid receptor?
MOP, KOP, NOP and DOP
68
What type of opioid receptor do all current drugs use?
µ receptors
69
What are the side effects of an opioid overdose?
``` °Respiratory depression °Sedation °Nausea/vomiting °Constipation °Itching °Immune suppression °Endocrine effects ```
70
What should you do when a patient is suffering from opioid induced respiratory depression?
°Call for help °Give oxygen °ABC °Naloxone
71
Why can codeine/tramadol be more/less effective in people?
It works by using the CYP2D6 gene which is over expressed in 5% of the population, leading to an increased risk of respiratory depression. Additionally, it is under-expressed/does not work in 20-25% of caucasians, leading to no effect
72
What are the two main neurotransmitter?
°Acetylcholine | °Noradrenaline
73
Which neurotransmitter do both sympathetic and parasymapthic fibres release and act on nicotinic receptors?
Acetylcholine
74
Which neurotransmitter do post-ganglionic parasympathetic fibres release?
Acetylcholine which acts on the muscarinic receptors
75
Which neurotransmitter do post-ganglionic sympathetic fibres release?
Noradrenaline which acts on alpha and beta adrenoreceptors
76
What do NANC (non-adrenergic, non-cholinergic autonomic transmitters) do?
They work on NO and vasoactive intestinal peptide (parasympathetic) and ATP and neuropeptide Y (sympathetic)
77
What/where are the muscarinic receptors?
``` °M1 = brain °M2 = mainly in the heart. Activation of M2 slows the heart so we can block these to reduce HR °M3 = glandular and smooth muscle. Cause bronchoconstriction, sweating, salivary gland secretion °M4/5 = mainly in CNS ```
78
Name a muscarinic agonist and list its effects
°Pilocarpine - Stimulation of salivation to treat Sjogren's - Contraction of smooth muscle to treat glaucoma - Slows the heart as a side effect
79
Name two muscarine antagonists and their origins
°Nightshade --> atropine | °Thorn apple --> hyoscine
80
Name one short acting and one long acting drug that can treat bronchoconstriction
°Work by blocking the M3 receptor °Short = ipratropium bromide °Long = LAMAs e.g. tiotropium
81
What effect does acetylcholine have outside of the autonomic nervous system?
°ACh signalling is involved in memory °Anti-emetic effects °ACh also helps to innervate skeletal muscle °Botox blocks the release of ACh
82
What are the side effects of anti-cholinergic medications?
``` °Worsening of memory °Constipation °Dry mouth °Vision (blurring and glaucoma) °Muscle paralysis (in the case of nerve gas) ```
83
What are the 3 catecholamines?
°Noradrenaline = released from sympathetic nerve fibre ends °Adrenaline = released from the adrenal glands °Dopamine
84
What is the most effective agonist of the α1 receptor, its mechanism and consequence of its activation?
°NAd>Ad °Increases intracellular calcium levels and Gq signalling °Contracts smooth muscle
85
What is the most effective agonist of the α2 receptor, its mechanism and consequence of its activation?
°NAd=Ad °Inhibits the cAMP family and used Gi signalling °Mixed effects on smooth muscle
86
What is the most effective agonist of the β1 receptor, its mechanism and consequence of its activation?
°NAd=Ad °Increases cAMP, Gs signalling °Chronotropic and inotropic effects on the heart
87
What is the most effective agonist of the β2 receptor, its mechanism and consequence of its activation?
°Ad>>NAd °Increases cAMP, Gs signalling °Relaxes smooth muscle
88
What is the most effective agonist of the β3 receptor, its mechanism and consequence of its activation?
°NAd>Ad °Increases cAMP, Gs signalling °Enhances lipolysis and relaxes detrusor muscle of the bladder
89
What do alpha antagonists do and why are they used?
°Causes vasoconstriction, especially in the skin and splanchnic region °Used to treat septic shock °Topical alpha activation can be used to relieve nasal decongestion
90
What do alpha blockers do?
°Blocking α1 decreased BP - doxazosin °Tamsulosin blocks α1A to treat prostatic hypertrophy °There are no useful α2 blockers
91
What do beta agonists do and why are they used?
°β1 activation increased heart rate °β2 activation can be life saving in asthma and delaying premature labour °β3 agonists reduce an overactive bladder
92
What are some beta blockers?
°Propanolol blocks β1+2 to slow HR, reduce tremors | °Atenolol is β1 selective and lowers BP
93
What are beta blockers used for?
``` °Angina °High BP °Arrhythmia °MI prevention °Anxiety °Heart failure ```
94
What is an adverse drug reaction?
An unwanted or harmful reaction following administration of a drug or combination of drugs under normal use and is suspected to be related to the drug
95
What are the three kinds of effect from an ADR?
°Toxic effect (dose > normal) °Collateral effect (dose = normal) °Hypersusceptibility (dose < normal)
96
What do each of the Rawlins-Thompson classifications mean?
°Type A (augmented) - they are predictable, dose dependant and common °Type B (bizarre) - non-predictable and not dose dependant °Type C (continuous) - chronic °Type D (delayed) - malignancies after immunosuppression °Type E (end of treatment) - withdrawal °Type F - failure of therapy
97
What are the risk factors for an ADR?
``` °Gender (F>M) °Age °Polypharmacy °Genes °Allergies °Hepatic/renal issue °Adherence ```
98
What are the causes of an ADR?
``` °Pharmaceutical variation in the drug °Receptor abnormality °Abnormal biological system which is revealed by the drug °Abnormalities in drug metabolism °Immunological causes °Drug interaction ```
99
What are the symptoms of anaphylaxis?
``` °Vasodilation °Increased vascular permeability °Bronchoconstriction °Urticaria °Angio-oedema °See ILA for more notes ```

Phase 2a (2 decks)

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